Active substanceOndansetronOndansetron
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  • Dosage form: & nbsp solution for intravenous and intramuscular administration
    Composition:

    1 ml of solution contains:

    Active substance: ondansetron hydrochloride dihydrate (in ondansetron) - 2 mg

    Excipients: citric acid, sodium citrate dihydrate, sodium chloride, water for injection.

    Description:

    Colorless or slightly colored transparent liquid.

    Pharmacotherapeutic group:Antiemetic means - serotonin receptor antagonist
    ATX: & nbsp

    A.04.A.A.01   Ondansetron

    Pharmacodynamics:

    Ondansetron is a selective receptor antagonist 5-HT3, (serotonin). Drugs for cytostatic chemotherapy and radiotherapy can cause an increase in the level of serotonin, which by activation of vagal afferent fibers containing receptors 5-HT3, causes a vomitive reflex. Ondansetron inhibits the appearance of a vomiting reflex by blockade of receptors 5-HT3 at the level of neurons of both the central and peripheral nervous system. Apparently, this mechanism of action is based on the prevention and treatment of post-operative and cytotoxic chemo- and radiotherapy-induced vomiting and nausea.

    Pharmacokinetics:

    With intramuscular injection, the peak concentration in plasma is reached within 10 minutes. The distribution of ondansetron is the same for intramuscular and intravenous administration.The drug is metabolized in the liver.

    The binding with plasma proteins is 70-76%. Less than 5% of the drug is excreted unchanged in urine.

    Half-life is about 3 hours, in elderly patients can reach 5 hours, and with severe hepatic insufficiency - 15-20 hours. With kidney damage (renal clearance less than 15 ml / min), the elimination half-life increases by 4-5 hours, but this increase is not clinically significant.

    Indications:

    Prevention and elimination of nausea and vomiting caused by cytostatic chemotherapy and radiotherapy, as well as postoperative nausea and vomiting.

    Contraindications:

    - Hypersensitivity to any component of the drug, pregnancy and lactation.

    - Children under 2 years of age (safety and efficacy have not been studied).

    Dosing and Administration:

    Cytostatic therapy

    The choice of dosage regimen is determined by the emetogenicity of antitumor therapy.

    For adults The daily dose, as a rule, is 8-32 mg, the following regimens are recommended.

    With moderate emetogenic chemotherapy or radiotherapy:

    - 8 mg intravenously struino slowly or intramuscularly, immediately before the start of therapy.

    With highly emeticogenic chemotherapy:

    - 8 mg intravenously struino slowly just before the start of chemotherapy, and then two more intravenous injections of 8 mg, each of which is carried out in 2-4 hours;

    - continuous 24-hour infusion of the drug at a dose of 24 mg at a rate of 1 mg / h;

    - 16-32 mg, diluted in 50-100 ml of the appropriate infusion solution, as a 15-minute infusion, immediately before the start of chemotherapy.

    The efficacy of ondansetron can be increased by a single intravenous injection of a glucocorticoid (eg, 20 mg of dexamethasone phosphate sodium salt) prior to chemotherapy.

    Children

    Children older than 2 years of the drug is administered at a dose of 5 mg / m2 surface of the body intravenously, immediately before the start of chemotherapy followed by oral administration at a dose of 4 mg after 12 hours.

    Prevention of postoperative nausea and vomiting

    Adults introduce a single dose of 4 mg intramuscularly or intravenously struino, slowly at the beginning of anesthesia.

    For relief of nausea and vomiting it is recommended intramuscular or slow intravenous injection of 4 mg of the drug.

    Intramuscularly in the same body region ondansetron can be administered at a dose not exceeding 4 mg!

    Children to prevent postoperative nausea and vomiting ondansetron is applied in a single dose of 0.1 mg / kg (maximum to 4 mg) in the form of a slow intravenous injection before or after anesthesia.

    To treat the development of postoperative nausea and vomiting in children, a slow intravenous injection of a single dose of the drug 0.1 mg / kg (maximum 4 mg) is recommended.

    With regard to the prevention and treatment of postoperative nausea and vomiting in children under the age of 2 years there is no sufficient experience.

    Elderly patients

    Dosage adjustments are not required.

    Patients with kidney and liver lesions

    With renal damage, the usual daily dose and frequency of administration of the drug is not required.

    With liver damage significantly reduces the clearance of ondansetron, and the half-life of it is increased from the plasma, so it is necessary to reduce the dose to 8 mg per day.

    To dilute the injection solution, the following solutions can be used:

    0.9% solution of sodium chloride,

    5% glucose solution, Ringer's solution,

    0.3% potassium chloride solution and 0.9% sodium chloride solution,

    0.3% potassium chloride solution and 5% glucose solution.

    Side effects:

    Allergic reactions: urticaria, bronchospasm, laryngospasm, angioedema, anaphylaxis.

    From the digestive system: hiccough, dry mouth, diarrhea, constipation, sometimes asymptomatic transient increase in the level of aminotransferases in the serum.

    From the side of the cardiovascular system: pain in the chest, in some cases with depression of the segment ST, arrhythmias, bradycardia, lowering blood pressure.

    From the nervous system: headache, dizziness, spontaneous movement disorders and convulsions.

    Local Reactions: pain, burning and redness at the injection site,

    Other: a flood of blood to the face, a feeling of heat, a temporary disturbance of visual acuity, hypokalemia.

    Overdose:

    In cases of suspected overdose, symptomatic therapy is indicated.

    The specific antidote is not known.

    Interaction:

    As ondansetron is metabolized by the enzyme system (cytochrome P450) of the liver, caution is required when combined:

    - with enzymatic inducers P450 (CYP2D6 and CYP3A) (barbiturates, carbamazepine, carisoprodol, glutethimide, griseofulvin, nitrous oxide, papaverine, phenylbutazone, phenytoin (probably other hydantoins), rifampicin, tolbutamide);

    - with inhibitors of enzymes P450 (CYP2D6 and CYP3A) (allopurinol, macrolide antibiotics, antidepressants - MAO inhibitors, chloramphenicol, cimetidine, oral contraceptives containing estrogens, diltiazem, disulfiram, valproic acid, sodium valproate, erythromycin, fluconazole, fluoroquinolones, isoniazid, ketoconazole, lovastatin, metronidazole, omeprazole, propranolol, quinidine, quinine, verapamil).

    Special instructions:

    In patients who previously had other selective 5HT antagonists3-receptors, there were observed hypersensitivity reactions, while Ondansetron-Ferein® can also develop similar reactions.

    As Ondansetron causes constipation, patients with signs of intestinal obstruction after using the drug require regular monitoring.

    The infusion solution should be prepared immediately before use. If necessary, the ready-made infusion solution can be stored for up to 24 hours at a temperature of 2-8 ° C.

    During the infusion, protection from light is not required; The diluted injection solution retains its stability at least infor 24 hours in natural light or normal lighting.

    Form release / dosage:

    Solution for intravenous and intramuscular administration 4 mg / 2 ml or 8 mg / 4 ml.

    Packaging:By 4 mg / 2 ml or 8 mg / 4 ml in ampoules of a neutral colorless or lightproof glass. For 5 ampoules - in a planar cell pack. 1 or 2 contour squares, together with instructions for use and a knife for opening ampoules or a scarifier ampoule or without a knife or scarifier - in a cardboard bundle.
    Storage conditions:

    In the dark place at a temperature of no higher than 30 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years

    The drug should not be used after the expiry date indicated on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:P N003200 / 01
    Date of registration:24.03.2010 / 28.04.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:BRYNTSALOV-A, CJSC BRYNTSALOV-A, CJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspBRYNTSALOV-A, CJSCBRYNTSALOV-A, CJSC
    Information update date: & nbsp07.06.2017
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